Identification of ß-Glucocerebrosidase Activators for Glucosylceramide hydrolysis

ChemMedChem. 2024 Feb 21:e202300548. doi: 10.1002/cmdc.202300548. Online ahead of print.ABSTRACTSeveral novel chemical series were identified that modulate glucocerebrosidase (GCase). Compounds from these series are active on glucosylceramide, unlike other known GCase modulators. We obtained GCase crystal structures with two compounds that have distinct chemotypes. Positive allosteric modulators bind to a site on GCase and induce conformational changes, but also induce an equilibrium state between monomer and dimer.PMID:38381042 | DOI:10.1002/cmdc.202300548

Source: ChemMedChem - February 21, 2024 Category: Chemistry Authors: Monika-Sarah E D Schulze Diana Scholz Eric Jnoff Adrian Hall Jonathan Melin Zara A Sands Elizabeth Rodriguez Veronique M Andre Source Type: research